Alkylating agents Flashcards

1
Q

Busulfan

AD VERSEEFFECT S

A

Severe myelosuppression (in almost all cases), pulmonary
fibrosis, hyperpigmentation

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2
Q

Busulfan

MECHANISM

A

Cross-links DNA

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3
Q

Nitrogen mustards
Cyclophosphamide,
ifosfamide

MECHANISM

A

Cross-link DNA
Require bioactivation by liver

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3
Q

Nitrogen mustards
Cyclophosphamide,
ifosfamide

AD VERSEEFFECT S

A

Myelosuppression, SIADH, Fanconi syndrome
(ifosfamide), hemorrhagic cystitis and bladder cancer
(prevent with mesna)

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4
Q

Nitrosoureas
Carmustine, lomustine

MECHAN ISM

A

Cross-link DNA Require bioactivation by liver
Cross blood-brain barrier

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5
Q

Nitrosoureas
Carmustine, lomustine

AD VERSEEFFECT S

A

CNS toxicity (convulsions,
dizziness, ataxia)

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6
Q

Procarbazine

mechanism

A

Mechanism unknown
Weak MAO inhibitor

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7
Q

procarbazine

adverseffect

A

Myelosuppression, pulmonary
toxicity, leukemia, disulfiramlike reaction

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8
Q

Temozolomide

mechanism

A

DNA methylation

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9
Q

Temozolomide

adverseffect

A

Myelosuppression

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10
Q

Platinum compounds
Cisplatin, carboplatin, oxaliplatin.

MECHANISM

A

Cross-link DNA. Cell cycle nonspecific.

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11
Q

Platinum compounds
Cisplatin, carboplatin, oxaliplatin.

AD VERSE EFFECT S

A

Nephrotoxicity (eg, Fanconi syndrome; prevent with amifostine), peripheral neuropathy, ototoxicity.

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12
Q

Taxanes
Docetaxel, paclitaxel

mechanism

A

Hyperstabilize polymerized microtubules → prevent mitotic spindle breakdown

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13
Q

Taxanes
Docetaxel, paclitaxel

AD VERSEEFFECT S

A

Myelosuppression, neuropathy,
hypersensitivity

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14
Q

Vinca alkaloids
Vincristine, vinblastine

mechanism

A

Bind β-tubulin and inhibit
its polymerization into
microtubules → prevent
mitotic spindle formation

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15
Q

Vinca alkaloids
Vincristine, vinblastine

adverseffect

A

Vincristine (crisps the nerves):
neurotoxicity (axonal
neuropathy), constipation
(including ileus)
Vinblastine (blasts the
marrow): myelosuppression

16
Q

Irinotecan, topotecan

mechanism

A

Inhibit topoisomerase I

17
Q

Irinotecan, topotecan

adverseffect

A

Severe myelosuppression,
diarrhea

18
Q

Etoposide, teniposide

mechanism

A

Inhibit topoisomerase II

19
Q

Etoposide, teniposide

adverseffects

A

Myelosuppression, alopecia

20
Q

Tamoxifen

mechanism

A

antagonist in breast tissue,
partial agonist in endometrium and bone

21
Q

Tamoxifen

adverseffects

A

Hot flashes, increase risk of thromboembolic events (eg, DVT, PE) and endometrial cancer.